5α-还原酶抑制剂对大鼠前列腺内雄激素的影响。

Effects of 5 alpha-reductase inhibitors on intraprostatic androgens in the rat.

作者信息

di Salle E, Giudici D, Biagini L, Cominato C, Briatico G, Panzeri A

机构信息

Experimental Endocrinology Department, R&D Oncology, Nerviano (MI), Italy.

出版信息

J Steroid Biochem Mol Biol. 1995 Jun;53(1-6):381-5. doi: 10.1016/0960-0760(95)00083-c.

DOI:10.1016/0960-0760(95)00083-c

PMID:7626485

Abstract

FCE 27837 is a novel inhibitor of 5 alpha-reductase, the enzyme responsible for the conversion of testosterone (T) to 5 alpha-dihydrotestosterone (DHT). The compound caused inhibition of human and rat prostatic enzymes, with IC50 values of 51 and 60 nM, respectively. The in vivo effect of FCE 27837 on 5 alpha-reductase was evaluated in adult male rats, treated orally at 10 mg/kg/day for 10 days. The compound caused 33 and 42% reductions in ventral prostate and seminal vesicle weights, respectively. The prostatic content of DHT, measured 6 h after the 10th dose of FCE 27837, was reduced by 75%, whereas T content increased by 442%. Similar effects were observed with 10 mg/kg/day of finasteride, whereas epristeride, tested at the same oral dose, was found to be the least effective compound, decreasing prostate weight by 22% and DHT content by 46%. Castration caused > 90% reductions in prostatic weight and prostatic DHT.

摘要

FCE 27837是一种新型5α-还原酶抑制剂，该酶负责将睾酮（T）转化为5α-双氢睾酮（DHT）。该化合物对人和大鼠前列腺酶均有抑制作用，其IC50值分别为51 nM和60 nM。在成年雄性大鼠中评估了FCE 27837对5α-还原酶的体内作用，大鼠口服给药，剂量为10 mg/kg/天，持续10天。该化合物使腹侧前列腺和精囊重量分别降低了33%和42%。在第10次给予FCE 27837后6小时测量，前列腺中DHT的含量降低了75%，而T含量增加了442%。以10 mg/kg/天的非那雄胺给药也观察到了类似的效果，而在相同口服剂量下测试的依立雄胺是效果最差的化合物，使前列腺重量降低了22%，DHT含量降低了46%。去势导致前列腺重量和前列腺DHT降低超过90%。